UY24498A1 - LACTAMA DERIVATIVES OF BENCIL AND BENCILIDENO AS AGONISTS AND SELTATIVE ANTAGONISTS OF 5-HT1A AND 5-HT1D RECEPTORS - Google Patents

LACTAMA DERIVATIVES OF BENCIL AND BENCILIDENO AS AGONISTS AND SELTATIVE ANTAGONISTS OF 5-HT1A AND 5-HT1D RECEPTORS

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Publication number
UY24498A1
UY24498A1 UY24498A UY24498A UY24498A1 UY 24498 A1 UY24498 A1 UY 24498A1 UY 24498 A UY24498 A UY 24498A UY 24498 A UY24498 A UY 24498A UY 24498 A1 UY24498 A1 UY 24498A1
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UY
Uruguay
Prior art keywords
disorders
hydrogen
antagonists
agonists
alkyl
Prior art date
Application number
UY24498A
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Spanish (es)
Inventor
Harry R Howard
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Pfizer
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Application filed by Pfizer filed Critical Pfizer
Publication of UY24498A1 publication Critical patent/UY24498A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36Oxygen or sulfur atoms
    • C07D207/382-Pyrrolones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32Oxygen atoms
    • C07D209/34Oxygen atoms in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74Oxygen atoms
    • C07D211/76Oxygen atoms attached in position 2 or 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
    • C07D211/86Oxygen atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente invención se refiere a derivados de lactama, a procedimientos y a intermedios para su preparación, a composiciones farmacéuticas que los contienen y a su uso en medicina. Los compuestos de la presente invención incluyen agonistas y antagonistas selectivos de receptores de serotonina 1 (5-HT1), específicamente, de uno o de los dos receptores 5-HT1A y 5-HT1D. Son útiles en el tratamiento o prevención de la migrana, depresión y otros trastornos para los que están indicados los agonistas o antagonistas de 5-HT1. Un compuesto de la fórmula (I) o una sal farmacéuticamente aceptable del mismo, en la que: R1 es un grupo de la fórmula G1, G2, G3, G4 ó G5, representados como figura 2, en las que E es oxígeno, azufre, SO o SO2; R2 es hidrógeno; R3 es (CH2)mB, donde m es 0, 1, 2 o 3 y B es hidrógeno, fenilo, naftilo, furilo, tienilo, piridilo, pirimidilo, tiazolilo, pirazolilo, isotiazolilo, oxazolilo, isoxazolilo, pirrolilo, triazolilo, tetrazolilo, imidazolilo, y donde cada uno de los grupos arilo y heteroarilo anteriores pueden estar opcionalmente sustituidos; Z es CR4R5, donde R4 y R5 se seleccionan independientemente entre hidrógeno, alquilo y trifluorometilo; ó Z puede ser furilo, tienilo, piridilo, pirimidilo, tiazolilo, pirazolilo, isotiazolilo, oxazolilo, isoxazolilo, pirrolilo, triazolilo, tetrazolilo, imidazolilo y donde dos miembros adyacentes en el anillo de Z también son miembros del anillo A; X es hidrógeno, cloro, fluoro, bromo, yodo, ciano, alquilo, hidroxi, trifluorometilo, alcoxi, Sog-alquilo donde g es 0, 1 o 2, CO2R10 ó CONR11R12; n es 1, 2, 3 o 4; y la línea discontinua indica un doble enlace opcional; con la condición de que n tiene qe ser 1 cuando Z es un grupo heteroarilo. Por ejemplo: 3-(2-(4-metilpiperazin-1-il)-bencilideno)-1,3-dihidro-indol-2-ona. Estos compuestos son útiles en un mamífero como agentes psicoterapéuticos, como ser en depresión, trastornos de ansiedad generalizada, fobias, pánico, Alzheimer, Parkinson, entre otros; para hipertensión disfunción sexual, trastornos de alimentación, obesidad, cefaleas, migranas, trastornos endocrinos, trastornos del tracto gastrointestinal, entre otras.The present invention relates to lactam derivatives, to processes and to intermediates for their preparation, to pharmaceutical compositions containing them and to their use in medicine. The compounds of the present invention include selective serotonin 1 (5-HT1) receptor agonists and antagonists, specifically, one or both of the 5-HT1A and 5-HT1D receptors. They are useful in the treatment or prevention of migraine, depression and other disorders for which 5-HT1 agonists or antagonists are indicated. A compound of the formula (I) or a pharmaceutically acceptable salt thereof, in which: R1 is a group of the formula G1, G2, G3, G4 or G5, represented as figure 2, in which E is oxygen, sulfur , SO or SO2; R2 is hydrogen; R3 is (CH2) mB, where m is 0, 1, 2 or 3 and B is hydrogen, phenyl, naphthyl, furyl, thienyl, pyridyl, pyrimidyl, thiazolyl, pyrazolyl, isothiazolyl, oxazolyl, isoxazolyl, pyrrolyl, triazolyl, tetrazolyl, imidazolyl, and where each of the above aryl and heteroaryl groups may be optionally substituted; Z is CR4R5, where R4 and R5 are independently selected from hydrogen, alkyl, and trifluoromethyl; or Z may be furyl, thienyl, pyridyl, pyrimidyl, thiazolyl, pyrazolyl, isothiazolyl, oxazolyl, isoxazolyl, pyrrolyl, triazolyl, tetrazolyl, imidazolyl and where two adjacent members in the ring of Z are also members of ring A; X is hydrogen, chlorine, fluoro, bromine, iodine, cyano, alkyl, hydroxy, trifluoromethyl, alkoxy, Sog-alkyl where g is 0, 1 or 2, CO2R10 or CONR11R12; n is 1, 2, 3 or 4; and the dashed line indicates an optional double bond; with the proviso that n has qe to be 1 when Z is a heteroaryl group. For example: 3- (2- (4-methylpiperazin-1-yl) -benzylidene) -1,3-dihydro-indole-2-one. These compounds are useful in a mammal as psychotherapeutic agents, such as in depression, generalized anxiety disorders, phobias, panic, Alzheimer's, Parkinson's, among others; for hypertension, sexual dysfunction, eating disorders, obesity, headaches, migraines, endocrine disorders, disorders of the gastrointestinal tract, among others.

UY24498A 1996-03-29 1997-03-21 LACTAMA DERIVATIVES OF BENCIL AND BENCILIDENO AS AGONISTS AND SELTATIVE ANTAGONISTS OF 5-HT1A AND 5-HT1D RECEPTORS UY24498A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US1513496P 1996-03-29 1996-03-29

Publications (1)

Publication Number Publication Date
UY24498A1 true UY24498A1 (en) 2000-09-29

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UY24498A UY24498A1 (en) 1996-03-29 1997-03-21 LACTAMA DERIVATIVES OF BENCIL AND BENCILIDENO AS AGONISTS AND SELTATIVE ANTAGONISTS OF 5-HT1A AND 5-HT1D RECEPTORS

Country Status (40)

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US (2) US6462048B2 (en)
EP (1) EP0894085B1 (en)
JP (1) JP3118467B2 (en)
KR (1) KR100305071B1 (en)
CN (1) CN1128788C (en)
AP (1) AP824A (en)
AR (1) AR006390A1 (en)
AT (1) ATE302182T1 (en)
AU (1) AU706839B2 (en)
BG (1) BG64176B1 (en)
BR (1) BR9708581A (en)
CA (1) CA2249603A1 (en)
CO (1) CO4650033A1 (en)
CZ (1) CZ293628B6 (en)
DE (1) DE69733996T2 (en)
DZ (1) DZ2198A1 (en)
EA (1) EA001485B1 (en)
ES (1) ES2246058T3 (en)
HK (1) HK1019446A1 (en)
HN (1) HN1997000023A (en)
HR (1) HRP970175A2 (en)
HU (1) HUP9902160A3 (en)
ID (1) ID17781A (en)
IL (1) IL125377A (en)
IS (1) IS4813A (en)
MA (1) MA26425A1 (en)
MY (1) MY118498A (en)
NO (1) NO312957B1 (en)
NZ (1) NZ325914A (en)
OA (1) OA10879A (en)
PL (1) PL329170A1 (en)
SK (1) SK131498A3 (en)
TN (1) TNSN97056A1 (en)
TR (1) TR199801929T2 (en)
TW (1) TW413679B (en)
UA (1) UA70284C2 (en)
UY (1) UY24498A1 (en)
WO (1) WO1997036867A1 (en)
YU (1) YU11997A (en)
ZA (1) ZA972690B (en)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH041367U (en) * 1990-04-13 1992-01-08
US6906093B2 (en) 1995-06-07 2005-06-14 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease
US6147106A (en) 1997-08-20 2000-11-14 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease
US5880141A (en) * 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US6696448B2 (en) * 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
US6423708B1 (en) * 1996-09-30 2002-07-23 Pfizer Inc Aralkyl and aralkylidene heterocyclic lactams and imides
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6531502B1 (en) 1998-01-21 2003-03-11 Sugen, Inc. 3-Methylidenyl-2-indolinone modulators of protein kinase
DE19830201A1 (en) * 1998-07-07 2000-01-13 Boehringer Ingelheim Pharma Antidepressant
CA2301899C (en) * 1998-07-27 2008-11-18 Boehringer Ingelheim Pharma Kg Agent with an antidepressant activity
US6624171B1 (en) 1999-03-04 2003-09-23 Smithkline Beecham Corporation Substituted aza-oxindole derivatives
GB9904933D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Compounds
US6492398B1 (en) 1999-03-04 2002-12-10 Smithkline Beechman Corporation Thiazoloindolinone compounds
EP1113015B1 (en) * 1999-12-29 2004-09-15 Pfizer Products Inc. Optically active 3-((2-piperazinyl-phenyl)methyl)-1-(4-(trifluoromethyl)-phenyl)-2-pyrrolidinone compounds as 5-HT1D receptor selective antagonists
US6620818B1 (en) 2000-03-01 2003-09-16 Smithkline Beecham Corporation Method for reducing the severity of side effects of chemotherapy and/or radiation therapy
MXPA04003385A (en) 2001-10-10 2005-04-11 Sugen Inc 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives as kinase inhibitors.
AU2003214800A1 (en) 2002-01-02 2003-07-24 Ardent Pharmaceuticals, Inc. Method of treating sexual dysfunctions with delta opioid receptor agonist compounds
TWI263497B (en) * 2002-03-29 2006-10-11 Lilly Co Eli Pyridinoylpiperidines as 5-HT1F agonists
DK1689721T3 (en) * 2003-11-26 2010-09-20 Pfizer Prod Inc Aminopyrazole derivatives as GSK-3 inhibitors
JP2007537151A (en) * 2004-01-29 2007-12-20 ファイザー・プロダクツ・インク Combination of γ-aminobutyric acid modulator and 5-HT1B receptor antagonist
AU2005223481A1 (en) 2004-03-17 2005-09-29 Pfizer Products Inc. Novel benzyl(idene)-lactam derivatives
CA2565996A1 (en) * 2004-05-11 2005-11-17 Pfizer Products Inc. Combination of atypical antipsychotics and 5-ht1b receptor antagonists
MXPA06012347A (en) * 2004-05-21 2007-01-17 Pfizer Prod Inc Pyrazinylmethyl lactam derivatives.
JP2008503559A (en) * 2004-06-25 2008-02-07 ファイザー・プロダクツ・インク Pyridylpiperazine for treating CNS disorders
ES2371927T3 (en) 2005-01-13 2012-01-11 Ge Healthcare Limited BENCIL-LACTAMA COMPOUNDS MARKED WITH 11C AND ITS USE AS IMAGE OBTAINING AGENTS.
WO2006106416A1 (en) * 2005-04-08 2006-10-12 Pfizer Products Inc. PYRIDIL-LACTAMS AND THEIR USE 5 -HTl RECEPTORS LIGAN
EP1891041A1 (en) * 2005-06-17 2008-02-27 Pfizer Products Incorporated METABOLITES OF 1- [-6- (1-ETHYL-l-HYDROXY-PROPYL) -PYRIDIN-3-YL]-3- [2- (4-METHYL-PIPERAZIN-I-YL) -BENZYL]-PYRR0LIDIN-2-0NE AS SERATONIN RECEPTOR ANTAGONISTS
WO2007012964A1 (en) * 2005-07-25 2007-02-01 Pfizer Products Inc. Preparation of alkylpiperazinylphenyl compounds by classical resolution
WO2007026224A2 (en) * 2005-08-31 2007-03-08 Pfizer Products Inc. 5-ht1b antagonist composition for depression, anxiety and cognition
WO2007026219A2 (en) * 2005-08-31 2007-03-08 Pfizer Products Inc. Combinations of a 5-ht1b antagonist with a noradrenalin re-uptake inhibitor or a serotonin noradrenalin reutake inhibitor for treating cns conditions
US20070096411A1 (en) * 2005-11-02 2007-05-03 Rempe Gary L Ii Device for retaining a kneeling rider on a gliding board
WO2014078568A1 (en) 2012-11-14 2014-05-22 The Johns Hopkins University Methods and compositions for treating schizophrenia
SI3344248T1 (en) 2015-09-02 2022-07-29 Trevena, Inc. 6-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same
BR112019016775A2 (en) 2017-02-17 2020-03-31 Trevena, Inc. DELTA-OPIOIDE MODULATING RECEIVER COMPOUNDS CONTAINING 7-MEMBER AZA-HETEROCYCLIC, METHODS OF USE AND PRODUCTION OF THE SAME
CN110520129A (en) 2017-02-17 2019-11-29 特维娜有限公司 Delta opiate receptor modulating compound and its use and preparation method containing 5 yuan of aza heterocycles
WO2020183011A1 (en) 2019-03-14 2020-09-17 Institut Curie Htr1d inhibitors and uses thereof in the treatment of cancer

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4078062A (en) * 1976-10-28 1978-03-07 E. R. Squibb & Sons, Inc. Substituted 2H-1,4-benzothiazin-3(4H)-ones
JPS62116557A (en) * 1985-11-15 1987-05-28 Takeda Chem Ind Ltd Substituted benzyl lactam
US5189179A (en) 1990-08-29 1993-02-23 Merrell Dow Pharmaceuticals Inc. Serotonin 5ht1a agonists
ES2162792T3 (en) 1991-09-18 2002-01-16 Glaxo Group Ltd BENZANILIDE DERIVATIVES AS 5-HT1D ANTAGONISTS.
AU2871592A (en) * 1991-10-11 1993-05-03 Du Pont Merck Pharmaceutical Company, The Cyclic ureas and analogues useful as retroviral protease inhibitiors
US5436246A (en) 1992-09-17 1995-07-25 Merrell Dow Pharmaceuticals Inc. Serotonin receptor agents
GB9410512D0 (en) * 1994-05-25 1994-07-13 Smithkline Beecham Plc Novel treatment
US5880141A (en) * 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US6467084B1 (en) * 1999-12-16 2002-10-15 Emware, Inc. Systems and methods for reprogramming an embedded device with program code using relocatable program code

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CZ305298A3 (en) 1999-07-14
AP824A (en) 2000-04-28
WO1997036867A1 (en) 1997-10-09
ID17781A (en) 1998-01-29
US20030027812A1 (en) 2003-02-06
NO312957B1 (en) 2002-07-22
HRP970175A2 (en) 1998-12-31
NZ325914A (en) 1999-09-29
US6462048B2 (en) 2002-10-08
AP9700955A0 (en) 1997-04-30
TNSN97056A1 (en) 2005-03-15
CZ293628B6 (en) 2004-06-16
CO4650033A1 (en) 1998-09-03
CN1214043A (en) 1999-04-14
JPH11506472A (en) 1999-06-08
CA2249603A1 (en) 1997-10-09
IL125377A (en) 2005-07-25
AU1317097A (en) 1997-10-22
NO984513L (en) 1998-09-28
MY118498A (en) 2004-11-30
US6924289B2 (en) 2005-08-02
HK1019446A1 (en) 2000-02-11
UA70284C2 (en) 2004-10-15
AR006390A1 (en) 1999-08-25
ATE302182T1 (en) 2005-09-15
EA199800771A1 (en) 1999-06-24
BG64176B1 (en) 2004-03-31
BG102791A (en) 1999-11-30
YU11997A (en) 1999-09-27
ZA972690B (en) 1998-09-28
PL329170A1 (en) 1999-03-15
IL125377A0 (en) 1999-03-12
EA001485B1 (en) 2001-04-23
BR9708581A (en) 1999-08-03
KR100305071B1 (en) 2001-12-12
OA10879A (en) 2001-10-05
HN1997000023A (en) 1997-06-05
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JP3118467B2 (en) 2000-12-18
KR20000005083A (en) 2000-01-25
TR199801929T2 (en) 1998-12-21
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TW413679B (en) 2000-12-01
EP0894085A1 (en) 1999-02-03
NO984513D0 (en) 1998-09-28
AU706839B2 (en) 1999-06-24
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HUP9902160A3 (en) 2001-02-28
DE69733996D1 (en) 2005-09-22
IS4813A (en) 1998-07-29
SK131498A3 (en) 2000-09-12
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US20020028821A1 (en) 2002-03-07
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CN1128788C (en) 2003-11-26

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